Anticancer sustained-released gel injection and preparation method thereof

Abstract

The invention relates to an anticancer slow-release gel injection and a preparation method thereof. The anticancer slow-release gel injection contains a taxane-like drug such as paclitaxel, docetaxel, hydroxypaclitaxel, epi-paclitaxel or deacetylpaclitaxel, a stine-like drug, an amphiphilic block polymer and a solvent. The composition exhibits the property of temperature-sensitive gelation, is a flowable liquid at the room temperature and turns into a stagnant and biodegradable water-insoluble gel in vivo in warm-blooded animals. The stine-like drug is selected from atrimustine, ambnmustine, nimustine, bendamustine, carmustine, elmustine, galamustine, fotemustine, estramustine, hesmustine, neptamustine, lomustine, semustine, ranimustine, semustine, tauromustine, tallimustine and spiromustine. The anticancer slow-release gel injection can release the drug slowly and locally around the tumor and retain the effective blood concentration for a plurality of weeks to a plurality of months, can not only kill tumor cells but also effectively inhibit tumor vessels, can reduce the general drug toxicity and can enhance the curative effect of chemotherapy particularly radioactive seed implantation.

Description

(1) Technical field [0001] The invention relates to an anti-cancer sustained-release gel injection and a preparation method thereof, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing taxanes and statins locally in solid tumors, mainly slow-release gel injections. It is an aqueous solution, which can become a semi-solid or solid gel in warm-blooded animals. (2) Background technology [0002] Although conventional chemotherapy has been used for a long time, its therapeutic effect on solid tumors is uncertain. Since the effect of chemotherapy depends on the action time and drug concentration of the drug at the tumor site, conventional chemotherapy cannot achieve the above goals. In addition, low doses of chemotherapeutic drugs can also induce drug resistance of tumor cells, and inappropriate chemotherapy can stimulate the proliferation and metastasis of tumors. [0003] Local appli...

AI Technical Summary

Problems solved by technology

Therefore, in most cases, the final sustained-release formulations are mostly solid shapes (eg, microspheres, tablets, or rods), which require a more complicated implantation process and are prone to tissue trauma and even tumor cell seeding or dissemination

In addition, organic solvents or high-heat processes often lead to the degradation and denaturation of many anti-cancer active ingredients, and solid implants cannot effectively cover the irregular tumor cavity after tumor resection, so residual tumor cells cannot be effectively removed after surgery.

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